雌激素受体显像剂<sup>18</sup>F-16α-17β-氟雌二醇的自动化合成

雌激素受体显像剂¹⁸F-16α-17β-氟雌二醇的自动化合成

摘要:
目的使用自动化合成装置Tracerlab FX_FN，制备雌激素受体显像剂¹⁸F-16α-17β-氟雌二醇（¹⁸F-FES）。
方法通过两步反应制备¹⁸F-FES：①¹⁸F^-和3-O-（甲氧甲基）-16, 17-O-磺酰基-16-表雌二醇发生亲核取代反应；②生成物经HCl水解，重复两次后得到产物¹⁸F-FES。
结果 ¹⁸F-FES的合成总时间约80 min，放化产率约为10%，放化纯度大于95%。
结论整个合成过程自动化完成，操作简便，¹⁸F-FES毒性小，对人安全，体外较稳定，有望成为安全、有效的雌激素受体显像剂。

Abstract:
Objective ¹⁸F-16α-17β-fluoroestradiol(¹⁸F-FES), an estrogen receptors imaging agent, is synthesized with Tracerlab FX_FNsystem.
Methods ¹⁸F-FES is obtained by two steps reactions, including the nucleophilic displacement reaction of no-carrier-added¹⁸F-fluoride with 3-O-methoxymethyl-16, 17-O-sulfuryl-16-epiesteriol, then the intermediate is evaporated and hydrolyzed with HCl and finally gives¹⁸F-FES.
Results The synthesis of¹⁸F-FES can be completed in about 80 min.The radiochemical yield and radio-chemical purity are about 10%and 95%respectively.
Conclusion The procedure ofsynthesis is simple and automatical.¹⁸FFES has an extremely lowtoxicity, which suggests that¹⁸F-FES may be a safe and effective estrogen receptors imagingagent.